Establishment of screening method for γ-aminobutyric acid transaminase inhibitor and its application in screening constituents in Gastrodiae Rhizoma / 中草药

ABSTRACT

Objective: To establish a screening model in vitro with γ-aminobutyric acid transaminase (GABA-T) as a target for screening the inhibitors of anti-epilepsy drugs for the treatment of nervous diseases and finish the structure-activity relationship analysis of p-hydroxybenzaldehyde as effective components in Gastrodiae Rhizoma and its analogs. Methods: Catalyst performed temperature, reaction time, the concentration of NAD+, α-ketoglutarate, and GABA were investigated to optimize the model. The test of p-hydroxybenzaldehyde (HBA) and its 11 analogs were selected as verification of this model. Results: The screening model in vitro based on GABA-T was established. The testing result of p-HBA and its 11 analogs was consistent with the practical activity recorded in the literature. Hydroxyl groups of -OH and -CHO in p-aldehyde on the benzene ring were pharmacophores. Conclusion: The model established in this paper can be used for high throughput screening the inhibitors of anti-epilepsy drugs, which provides the reference for the study on the inhibitors of anti-epilepsy drugs for nervous diseases and their mechanisam.